The present invention relates to a novel composition, in particular pharmaceutical composition, for use as laxative (also referred to synonymously as “cathartic” or “purgative”) and to a method for its manufacture, and to the use of this composition as laxative (i.e. cathartic or purgative).
Laxatives—also referred to synonymously as “purgatives” or “cathartics”—exist in very diverse forms, including numerous herbal cathartics.
Thus, for example, the use of plantago seed (plantaginis ovatae semen or semen plantaginis ovatae, also called synonymously Indian plantain, Indian psyllium, blond psyllium, ispaghula or semen ispaghulae) and/or its seed husks (plantago seed husks, plantaginis ovatae seminis integumentum) for medicaments for regulating bowel activity is known. Plantago seed has a considerable swelling ability and exerts a physical expansion stimulus on the sensitive receptors of the bowel walls. In a known method (cf. German patent 11 03 520), the seeds are finely ground, made into a viscous paste with water and dried in strand form, comminuted and finally coated.
The effect of the senna plant (senna plant, Cassia senna L. and Cassia angustifolia Vahl), especially its fruits (fructus sennae, also referred to synonymously as senna pods) (e.g. Alexandria senna fruits=sennae fructus acutifoliae and/or Tinnevelly senna fruits=sennae fructus angustifoliae) and their fruit husks as well as their leaves (folia sennae), as herbal cathartic is likewise known.
Laxatives which combine the two aforementioned action principles are also known, for example laxatives in which the physical effect of plantago seeds is supported by the pharmacologically stimulating action principle of the sennosides, the constituents of senna fruits, in order to achieve a better overall effect.
Thus, mixtures of ground plantago seeds and senna fruits as a simple mixture in which the constituents are present side by side have previously been disclosed. However, the flow-ability and suspendability in water cannot be optimally adjusted with such mixtures, but this would be desirable for oral administration. Processing of these mixtures to powders ready for administration is moreover impossible or not directly possible.
In order to remedy the aforementioned disadvantages, DE 30 01 357 C2 proposed a laxative in the form of cathartic granules based on senna fruits, plantago seeds and, where appropriate, plantago seed husks with an increased release-slowing effect, where the senna particles are enveloped or encased by plantago seeds, especially gummy substances of the plantago seeds. The composition described therein is an efficient laxative. However, since the composition is in the form of granules with a particle size of about 1 mm to about 3 mm of the granule particles, i.e. of asymmetric aggregates of powder particles, it must be taken with copious water. Otherwise there is the risk on inappropriate oral intake or administration, i.e. on oral intake or administration with amounts of water which are too small, that swollen lumps of the granules may form and may, in the worst cases, lead to blockage of the esophagus or else even of the gastrointestinal tract.
Laxatives which are based on plantains or Indian plantains (psyllium) or their constituents and which are on the market often do not have a sufficient cathartic effect and, after suspension in water, because of the rapid onset of the swelling effect of the plantain, do not remain drinkable for long, so that they must be taken immediately after preparing the aqueous suspension. This is because, after suspension in water, these products form a gel after only a few minutes and produce a thick, undrinkable agglomerate on the surface. In addition, with most of the products there is very rapidly at least a two-layer phase separation which no longer ensures homogeneous distribution of the active components in the stirred product. These products must also be taken with copious water because, otherwise, there is a risk of the possible formation of swollen agglomerates which, in the worst cases, may lead to blockage of the esophagus or else even of the gastrointestinal tract. Further disadvantages of these products are also the insipid taste and the artificial appearance.
In addition, DE 103 46 083 A1, which derives from the applicant, and the parallel documents belonging to the same patent family, WO 2005/027948 A1 and US 2005/0053676 A1, describe a laxative based on a powdered composition which, besides plantago seeds (plantaginis ovatae semen) and/or plantago seed husks and at least one anthranoid compound with a cathartic effect, in particular at least one sennoside, preferably in the form of anthranoid- or sennoside-containing plant constituents/parts, also comprises at least one polygalactomannan-based polysaccharide or derivative thereof, in particular guaran (guar gum). The latter acts firstly as (co)stabilizer in an aqueous suspension of the powdered composition, and secondly cooperates, especially because of its swelling ability, synergistically with the other components of the composition by assisting the cathartic effect thereof, and additionally facilitates the processability of the composition of the invention to a fine-particle powder which can be directly dispersed in water. However, an additional component, namely the polygalactomannan-based polysaccharide or derivative thereof, is necessary in the aforementioned composition in order to achieve the desired properties. It is also possible in some cases to employ relatively high dosages. Moreover, the aforementioned composition by its nature as a powder is associated with a high dust content.
U.S. Pat. No. 4,511,561 A which likewise derives from the applicant describes a laxative in the form of granules which, besides plantago seeds (plantaginis ovatae semen) and/or plantago seed husks and senna fruits, also comprises gum tragacanth.